抗艾滋病新类型复方制剂Evotaz tablet(ATAZANAVIR SULFATE; COBICISTAT)获FDA批准上市 EVOTAZ™(阿扎那韦和cobicistat)片剂为口服药 美国首次批准:2015年5月6日 公司:百时美施贵宝 目前的主要变化 警告和注意事项, 严重不良反应或病毒学的流失风险 应对由于药物相互作用 适应症和用法 EVOTAZ是一个组合的人类免疫缺陷病毒(HIV-1)蛋白酶抑制剂和抑制CYP3A为表示与其他抗逆转录病毒药物对HIV-1感染的治疗联合使用。 【用法用量】 •建议用量成人:每日一片一次,口服食物一起服用。 剂型和规格 •片剂:300mg的阿扎那韦和150mg cobicistat。
EVOTAZ Rx Pharmacological Class: HIV-1 protease inhibitor + CYP3A inhibitor.
Active Ingredient(s): Atazanavir 300mg, cobicistat 150mg; tablets.
Company Bristol-Myers Squibb , sildenafil (for PAH), indinavir.
Warnings/Precautions: Assess CrCl prior to initiation. When concomitant tenofovir DF: assess baseline CrCl, urine glucose, and urine protein; if CrCl <70mL/min: not recommended; monitor serum phosphorous if risk of renal impairment. ESRD with hemodialysis in treatment-experienced or hepatic impairment: not recommended. Cardiac conduction abnormalities; consider ECG monitoring if preexisting marked 1st -degree AV block or 2nd/3rd -degree AV block. Consider interruption or discontinuation if nephrolithiasis or cholelithiasis occurs. Hepatitis B and/or C or marked elevations in transaminases: monitor LFTs before and during therapy. Consider alternative if jaundice or scleral icterus occurs. Diabetes. Hyperbilirubinemia. Fat redistribution. Immune reconstitution syndrome. Hemophilia. Elderly. Pregnancy (Category B). Nursing mothers: not recommended.
Interaction(s) See Contraindications. Separate dosing with concomitant H2 receptor antagonists, PPIs (not recommended in treatment-experienced), antacids, enteric-coated didanosine. Concomitant tenofovir DF with concomitant or recent nephrotoxic agents, other antiretrovirals that require CYP3A inhibition (eg, HIV protease inhibitors, elvitegravir), atazanavir- or cobicistat-containing products, ritonavir, CYP2C8 substrates with narrow therapeutic indices (eg, paclitaxel, repaglinide), efavirenz, etravirine, apixaban, rivaroxaban, dabigatran etexilate, avanafil, inhaled/nasal steroids, salmeterol, voriconazole: not recommended. May need to adjust dose of insulin, antidiabetics, dasatinib, nilotinib, sildenafil, tadalafil, vardenafil, perphenazine, risperidone, thioridazine, buprenorphine, naloxone, methadone, tramadol, bosentan, rifabutin, and sedatives/hypnotics. Concomitant maraviroc: give maraviroc 150mg twice daily. Monitor concomitant antiarrhythmics, digoxin, vincristine, vinblastine, warfarin, clonazepam, carbamazepine, lamotrigine, SSRIs, TCAs, trazodone, fentanyl, immunosuppressants, other statins, β-blockers, CCBs. Concomitant macrolide or ketolide antibiotics, CYP3A-inducing anticonvulsants, systemic corticosteroids: consider alternatives.
Adverse Reaction(s) Jaundice, ocular icterus, nausea; rash (may be severe).
How Supplied: Tabs—30
LAST UPDATED: 6/5/2015 百时美施贵宝抗HIV新药Evotaz获FDA批准 近日,百时美施贵宝宣布其新药 Evotaz获FDA批准, Evotaz 是atazanavir、cobicistat和其它抗病毒药的固定剂量复方制剂,用于治疗成人艾滋病。Evotaz为片剂,用法是每日一次,由300mg的 atazanavir(一种蛋白酶抑制剂,以商品名Reyataz 单独销售)、150mg的 cobicistat(据称是一种“增强药代动力学”的药物,目前由吉利德以商品名Tybost销售)组成。Evotaz获批对HIV感染者而言是一个好消息。据悉每年约有50000人感染HIV而导致获得性免疫缺陷综合征(AIDS)。目前美国的HIV感染者约为110万人,而大多数患者对治疗有耐药性,因此需要新的治疗方法来抑制病毒。FDA批准Evotaz是基于称为114号研究的3期临床试验的阳性结果。该双盲试验比较了300mg Reyataz+150mg cobicistat (即Evotaz)和300mg Reyataz+100mg ritonavir 的效果。48周治疗后,服用Evotaz的病人中85%的HIV-1 RNA水平低于50个拷贝/ml,与对照组Reyataz/ritonavir的87%消退率相比是不分伯仲。此外,Evotaz作为蛋白酶抑制剂单独使用时抗病毒的失效率低于6%,与cobicistat联用后,失效率就降到最低。最重要的是,临床试验结果表明48周后病人的耐药性为零,单独用tenofovir无耐药性,而当用Evotaz 后病人表现出对 emtricitabine有耐药性。但是总体而言,3期临床结果表明了 Evotaz的有效性和安全性。百时美施贵宝的全球市场总管Murdo Gordon表示, 百时美很高兴能为全球AIDS患者提供新的治疗方法,atazanavir与cobicistat 联用能维持48周以上安全、有效的治疗。此番Evotaz获批标志着一个开创性的治疗方式。然而,Evotaz和Reyataz并不代表能完全治愈HIV-1感染造成的AIDS。并且那些接受 Evotaz 治疗的患者此前也接受过其他的抗病毒治疗,一定程度上已经获得了蛋白酶抑制剂治疗的耐药性“基线”水平。此外对Evotaz任意一种成分过敏的患者也不能用药。 |